A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the α and β isoforms (IC₅₀ = 44 nM), but not the γ or δ isoforms (IC₅₀ >100 µM) of p38 MAP kinase. Inhibits IL-1 and TNF-a production in LPS-stimulated human peripheral blood monocytes (IC₅₀ = 120 nM and 350 nM, respectively). Reported to protect against mild excitotoxic neuronal injury caused by NMDA and provides substantial protection against cell death induced by either oxygen glucose deprivation (OGD) or magnesium deprivation in cultured neurons. Also reported to reduce myocardial reperfusion injury via inhibition of endothelial adhesion molecule expression and blockade of polymorphonuclear (PMN) accumulation.

Cell permeable: yes

Primary Target
MAPKp38α & β

Product competes with ATP.

Reversible: yes

Target IC₅₀: 44 nM against of the α- and β-isoforms of MAP kinase p38; <100 µM against the γ- or δ-isoform of MAP kinase p38

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

May require slight warming to achieve complete solubilization.

Gao, F., et al. 2002. Cardiovasc. Res.53, 414.
Ju, H., et al. 2002. J. Pharmacol. Exp. Ther.301, 15.
Legos, J.J., et al. 2002. Eur. J. Pharmacol.447, 37.
Barone, F.C., et al. 2001. J. Pharmacol. Exp. Ther.296, 312.
Ward, K.W., et al. 2001. Pharm. Res.18, 1336.
Underwood, D.C., et al. 2000. J. Pharmacol. Exp. Ther.293, 281.
Underwood, D.C., et al. 2000. Am. J. Physiol. Lung Cell Mol. Physiol.279, L895.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)